Trospium chloride is an agent that has been known for several decades (cf. German patent 1 194 422) as an anticholinergic that is useful, for example, as a spasmolytic agent. This active agent has been available as an orally administrable, solid administration form (tablets and dragees), for intravenous or intramuscular injection as an injection solution and for rectal administration as suppositories and is mainly used for the treatment of bladder dysfunctions (urge incontinence, detrusorhyperreflexia). When these administration forms are used, losses of trospium chloride occur during the transport of the agent from the administration point to the action point. These losses are due to the excretion and metabolism processes occurring during systematic passage. In the case of the oral and rectal administration forms, losses are also due to poor absorption of trospium chloride, a quaternary ammonium compound, from the intestinal lumen into the system. In addition, with such active agent administration types, the typical side effects for anticholinergics, such as heart rate increases, dryness of the mouth, accommodation difficulties, etc. become disadvantageously noticeable.
Other anticholinergics, which as a result of their molecular structure constitute tertiary amines (e.g. oxybutynin), are absorbed to a greater extent following intravesicular instillation than following the administration of equivalent oral dosages (Massad C. A., Kogan B. A. & Trigo/Rocha F. E.: The Pharmacokinetics of intravesical and oral oxybutynin chloride. J. Urol. 148: 595/597, 1992). Thus, intravesical instillation of tertiary amine anticholinergics will not limit undesired anticholinergic side effects, because intravesicular absorption of tertiary amines will result in systemic effects at the target organ (e.g., heart, salivary gland, eye).
The problem to be solved by the present invention is consequently to prevent the disadvantages of the existing trospium administration forms, but still provide for administration by the patient, so that there is no need for clinical personnel or a doctor.